Current methods for oral delivery of macromolecular and other drugs poorly absorbed by the intestine do not provide adequate oral bio-availability. Thus, new intestinal pathways to transport larger quantities of compound must be identified. Unfortunately, current methods of pathway identification are inadequate. XenoPort will address this problem by developing a new method for displaying synthetic molecules on phage particles to fully exploit the exquisite sensitivity and versatility of the phage for display of molecular libraries. These libraries then will be used to screen for ligands to receptors directing the most active transcytosis pathways through the intestinal epithelium, enabling development of a commercial-ready technology platform adaptable to a wide variety of compounds in all therapeutic areas. Phase I studies will demonstrate feasibility by synthesizing, characterizing, and attaching a 1000-member chemical library to phage, and selecting for active compounds. Phase II will develop a highly diverse, 100,000-member library that also will be validated by selection of biologically active, synthetic molecules. The technology will be commercialized via internal product development and strategic partnerships. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE